公开(公告)号：US4806527A

公开(公告)日：1989-02-21

申请号：US26409

申请日：1987-03-16

申请人： Burton G. Christensen ,  Helmut Mrozik ,  Michael H. Fisher

发明人： Burton G. Christensen ,  Helmut Mrozik ,  Michael H. Fisher

IPC分类号： C07D493/22 ,  A01N43/90 ,  A61K31/365 ,  A61P33/00 ,  C07H17/08 ,  C07H19/01 ,  A61K31/70 ,  C07D313/06 ,  C07H17/04

CPC分类号： C07H19/01 ,  A01N43/90

摘要： There are disclosed derivatives of avermectin compounds with a .DELTA.26,27-alkyl chain of 4, 5 or 6 members at the 25-position. The compounds are prepared from the known .DELTA.26,27-compounds by the appropriate synthetic procedures at the 5-, 8-, 9-, 13- , 22- and 23-positions. The compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

公开(公告)号：US5606054A

公开(公告)日：1997-02-25

申请号：US166440

申请日：1993-12-14

申请人： Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen ,  Thomas L. Shih ,  Matthew J. Wyvratt

发明人： Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen ,  Thomas L. Shih ,  Matthew J. Wyvratt

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  A61K31/55

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.

摘要翻译： 公开了鉴定为杂环稠合内酰胺的某些新化合物，其促进人和动物中生长激素的释放。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身高。 还公开了含有这样的杂环稠合内酰胺作为其活性成分的生长促进组合物。

公开(公告)号：US5284841A

公开(公告)日：1994-02-08

申请号：US13448

申请日：1993-02-04

申请人： Lin Chu ,  Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen

发明人： Lin Chu ,  Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen

IPC分类号： A61K31/55 ,  A61P3/00 ,  A61P3/02 ,  A61P3/04 ,  A61P5/00 ,  A61P43/00 ,  C07D223/16 ,  C07D403/10 ,  C07D403/14 ,  C07D409/06 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07K5/06 ,  C07D209/34 ,  C07D215/227

CPC分类号： C07D223/16 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07K5/06

摘要： There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

摘要翻译： 公开了一些确定为促进人和动物中生长激素释放的苯并稠合内酰胺的新化合物。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身材。 通过用取代的酰胺官能团取代氨基 - 内酰胺来制备化合物。 还公开了含有这样的苯并稠合内酰胺作为其活性成分的生长促进组合物。

公开(公告)号：US5789587A

公开(公告)日：1998-08-04

申请号：US744296

申请日：1996-11-06

申请人： Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen ,  Thomas L. Shih ,  Matthew J. Wyvratt

发明人： Michael H. Fisher ,  Helmut Mrozik ,  William R. Schoen ,  Thomas L. Shih ,  Matthew J. Wyvratt

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  A61K31/55

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.

摘要翻译： 公开了鉴定为杂环稠合内酰胺的某些新化合物，其促进人和动物中生长激素的释放。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身高。 还公开了含有这样的杂环稠合内酰胺作为其活性成分的生长促进组合物。

公开(公告)号：US5015630A

公开(公告)日：1991-05-14

申请号：US298710

申请日：1989-01-19

申请人： Michael H. Fisher ,  Helmut Mrozik

发明人： Michael H. Fisher ,  Helmut Mrozik

IPC分类号： A01N43/90 ,  A01N47/34 ,  A01N55/00 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07D493/22 ,  C07F7/18 ,  C07H17/08 ,  C07H19/01

CPC分类号： C07H19/01 ,  C07H17/08

摘要： Novel avermectin derivatives are disclosed, wherein the 5-hydroxy group is replaced by an oxime group. The avermectin-5-oximes can further be derivatized at the 4"- or 4'-positions as amino, substituted amino, acylhydrazone, semicarbazone, or substituted semicarbazone analogues. The avermectin-5-oximes are prepared by the oxidation of the 5-hydroxy compounds with manganese dioxide or with pyridinium dichromate to the known 5-oxo analogues, and these are then reacted with a hydroxylamine salt. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

公开(公告)号：US5008250A

公开(公告)日：1991-04-16

申请号：US198271

申请日：1988-05-25

申请人： Michael H. Fisher ,  Matthew J. Wyvratt ,  Helmut Mrozik

发明人： Michael H. Fisher ,  Matthew J. Wyvratt ,  Helmut Mrozik

IPC分类号： C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  A61P33/00 ,  A61P33/10 ,  C07D493/20 ,  C07D493/22 ,  C07H19/01

CPC分类号： C07H19/01 ,  A01N43/90

摘要： There are disclosed novel avermectin compounds having a cleaved furan ring and a hydroxy group in the 8a position. Processes for preparing these novel compounds are also disclosed. These compounds have utility as anti-parasitic agents and as insecticides against agricultural pests.

公开(公告)号：US5350742A

公开(公告)日：1994-09-27

申请号：US74763

申请日：1993-06-10

申请人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

发明人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

IPC分类号： C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/366 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

CPC分类号： C07H19/01 ,  A01N43/90

摘要： Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

摘要翻译： 公开了阿维菌素衍生物，其在4'单糖位置，4“二糖位置或23位置引入两个氟原子。 还公开了阿维菌素糖苷配基衍生物，其在13或23位上引入两个氟原子。这些二氟阿维菌素类似物衍生自相应的酮和烯酮，其又通过天然存在的阿凡曼菌素的化学修饰来制备。 这些化合物在人和动物中用作止痛药，杀虫剂和抗脑炎药，还公开了含有其活性成分的化合物的组合物。

公开(公告)号：US5229416A

公开(公告)日：1993-07-20

申请号：US875486

申请日：1992-04-29

申请人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

发明人： Peter T. Meinke ,  Helmut Mrozik ,  Michael H. Fisher

IPC分类号： C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/366 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/00 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

CPC分类号： C07H19/01 ,  A01N43/90

摘要： Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

摘要翻译： 公开了阿维菌素衍生物，其在4'单糖位置，4“二糖位置或23位置引入两个氟原子。 还公开了阿维菌素糖苷配基衍生物，其在13或23位上引入两个氟原子。这些二氟阿维菌素类似物衍生自相应的酮和烯酮，其又通过天然存在的阿凡曼菌素的化学修饰来制备。 这些化合物在人和动物中用作止痛药，杀虫剂和抗脑炎药，还公开了含有其活性成分的化合物的组合物。

公开(公告)号：US07125873B2

公开(公告)日：2006-10-24

申请号：US10481353

申请日：2002-07-05

申请人： Scott D Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E Weber ,  Jinyou Xu

发明人： Scott D Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E Weber ,  Jinyou Xu

IPC分类号： A61K31/44

CPC分类号： A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US06399786B1

公开(公告)日：2002-06-04

申请号：US09901264

申请日：2001-07-09

申请人： Steven L. Colletti ,  Michael H. Fisher ,  Peter T. Meinke ,  Matthew J. Wyvratt

发明人： Steven L. Colletti ,  Michael H. Fisher ,  Peter T. Meinke ,  Matthew J. Wyvratt

IPC分类号： A61K31407

CPC分类号： C07D491/16 ,  A01N43/90 ,  C07D491/22

摘要： The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

摘要翻译： 本发明涉及杀螨，抗寄生虫，杀虫剂和驱肠虫剂的新型节肢动物酸衍生物。